Abstract
The major inhibitory neurotransmitter, γ-aminobutyric acid (GABA) acts on a postsynaptic receptor complex which includes GABA and benzodiazepine (BZ) recognition sites and a chloride ionophore (Turner and Whittle, 1983). Pharmacological, biochemical and neurophysiological studies suggest that BZ agonists, such as diazepam, exert their central effects by enhancing lowaffinity GABA binding (DeFeudis, 1983; Olsen and Venter, 1986).
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References
Anton-Tay, F., 1974, Melatonin: effects on brain function, Adv. Biochem. Psychopharmacol., 11: 315–324.
Anton-Tay, F., Diaz, J.L. and Fernandez-Guardiola, A., 1971, On the effect of melatonin upon human brain: its possible therapeutic implications, Life Sci., 10: 841–850.
Coloma, F.M., and Niles, L.P., 1988, Melatonin enhancement of [3H]-7-aminobutyric acid and [3H]muscimol binding in rat brain, Biochem. Pharmacol., 37: 1271–1274.
Concas, A., Serra, M., Atsoggiu, T., and Biggio, G., 1988, Foot-shock stress and anxiogenic ß-carbolines because of t-[35S]buty1bicyclo-phosphorothionate binding in the rat cerebral cortex, an effect opposite to anxiolytics andγ-aminobutyric acid mimetics, J. Neurochem., 51: 1868–1876.
DeFeudis, F.V., 1983, Psychoactive agents and GABA-receptors, Pharmacol. Res. Comm., 15: 29–39.
Gee, K.W., 1987, Phenyquinolines PK8165 and PK9084 allosterically modulate [35S]t-butybicyclophosphorothionate binding to a chloride ionophore in rat brain via a novel Ro5 4864 binding site, J. Pharmacol. Exp. Ther., 240: 747–753.
Gee, K.W., Lawrence, L.J., and Yamamura, H.I., 1986, Modulation of the chloride ionophore by benzodiazepine receptor ligands: influence GABA and ligand efficacy, Mol. Pharmacol., 30: 218–225.
Haefely, W.E., 1989, Pharmacology of the allosteric modulation of GABAA receptors by benzodiazepine receptor ligands, in: “Allosteric Modulation of Amino Acid Receptors: Therapeutic Implications”, Barnard, E.A., and Costa, E., eds., Raven Press, New York, pp. 47–69.
Holmes, S.W., and Sugden, D., 1982, Effects of melatonin on sleep and neurochemistry in the rat, Br. J. Pharmacol., 76: 95–101.
Honoré, T., and Drejer, J., 1985, Phenobarbitone enhances [35S]TBPS binding to extensively washed rat cortical membranes, J. Pharm. Pharmacol., 37: 928–929.
Marangos, P.J., Patel, J., Boulenger, J.-P., and Clark-Rosenberg, R., 1982, Characterization of peripheral-type benzodiazepine binding sites in brain using [3H]Ro5-4864, Mol. Pharmacol., 22: 26–32.
Marangos, P.J., Patel, J., Hirata, F., Sondhein, D., Paul, S.M., Skolnick, P., and Goodwin, F.K., 1981, Inhibition of diazepam binding by tryptophan derivatives including melatonin and its brain metabolite N-acetyl-5-methoxykynurenamine, Life Sci., 29: 259–267.
Niles, L.P., Pickering, D.S., and Arciszewski, M.A., 1987, Effects of chronic melatonin administration on GABA and diazepam binding in rat brain, J. Neural Transm., 70: 117–124.
Olsen, R.W., and Venter, J.C., 1986, “Benzodiazepine-GABA Receptors and Chloride Channels: Structural and Functional Properties”, Alan R. Liss, New York.
Romijn, H.J., 1978, The pineal, a tranquilizing organ? Life Sci., 23: 2257–2274.
Squires, R.F., Casida, J.E., Richardson, M., and Saederup, E., 1983, 35S-t-Butylbicyclophosphorothionate binds with high affinity to brainspecific sites coupled to γ-aminobutyric-A and ion recognition sites, Mol. Pharmacol., 23: 326–336.
Sugden, D., 1983, Psychopharmacological effects of melatonin in mouse and rat, J. Pharmacol. Exp. Therap., 227: 587–591.
Tehrani, M.H.J., Vaidyanathaswamy, R., Verkade, J.G., and Barnes, E.M. Jr., 1986, Interaction of t-butylbicyclophosphorothionate with γ-aminobutyric acid-gated chloride channels in cultured cerebral neurons, J. Neurochem., 46: 1542–1548.
Turner, A.J., and Whittle, S.R., 1983, Biochemical dissection of the γ-aminobutyrate synapse, Biochem. J., 209: 29–41.
Van Renterghem, C., Bilbe, G., Moss, S., Smart, T.G., Constanti, A., Brown, D.A., and Barnard, E.A., 1987, GABA receptors induced in xenopus oocytes by chick brain mRNA: evaluation of TBPS as a use-dependent channel blocker, Mol. Brain Res., 2: 21–31.
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© 1991 Plenum Press, New York
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Niles, L. (1991). Melatonin Interaction with the Benzodiazepine-GABA Receptor Complex in the CNS. In: Schwarcz, R., Young, S.N., Brown, R.R. (eds) Kynurenine and Serotonin Pathways. Advances in Experimental Medicine and Biology, vol 294. Springer, Boston, MA. https://doi.org/10.1007/978-1-4684-5952-4_24
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DOI: https://doi.org/10.1007/978-1-4684-5952-4_24
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